LY3009120

SKU: orb1300380

Description

LY3009120 is a potent pan-Raf inhibitor, demonstrating IC50 values of 44 nM, 31-47 nM, and 42 nM against A-Raf, B-Raf, and C-Raf, respectively, in A375 cell assays. This investigational compound has been evaluated in Phase 1 clinical trials for its potential in oncology research, supporting studies into MAPK pathway signaling in both cellular and in vivo models.

Research Area

Cell Biology, Signal Transduction

Key Properties

• CAS Number: 1454682-72-4
• MW: 424.51
• Purity: 99.76% (May vary between batches)
• Formula: C₂₃H₂₉FN₆O
• SMILES: CNc1ncc2cc(c(C)nc2n1)-c1cc(NC(=O)NCCC(C)(C)C)c(F)cc1C
• Target: Raf,Autophagy
• Solubility: DMSO:10 mg/mL (23.56 mM)

Bioactivity

• Target IC50:
  B-Raf (V600E):5.8 nM|B-Raf (WT):15 nM|B-Raf:9.1 nM|C-Raf:4.3 nM
• In Vivo:
  In rats bearing BRAF V600E ST019VR PDX tumors, LY3009120 (15 or 30 mg/kg, p.o.) shows a dose-dependent tumor growth inhibition. In nude rats bearing A375 xenograft, single dose oral treatment with LY3009120 (3 to 50 mg/kg, p.o.) shows a dose dependent inhibition of phospho-ERK, with a dose for 50% inhibition of phospho-ERK (EC50) of 4.36 mg/kg, with plasma concentration to achieve 50% inhibition of phospho-ERK (EC50) of 68.9 ng/mL or 165 nM.
• In Vitro:
  LY3009120 inhibits the cell growth of A375 and HCT116 cells with the IC50 of 9.2 and 220 μM, respectively. LY3009120 inhibits the tyrosine kinase KDR with the IC50 of 3.9 μM.
• Cell Research:
  Brie y, cells are grown in DMEM high glucose supplemented with 10% characterized fetal bovine serum and 1% penicillin/streptomycin/L -glutamine at 37℃, 5% CO2, and 95% humidity. Cells are allowed to expand until 70-95% con uency. A serial dilution of test compound is dispensed into a 384-well black clear bottom plate. 625 cells are added per well in 50 μL of complete growth medium. Plates are incubated for 67 h at 37℃, 5% CO2 , and 95% humidity. Then, 10 μL of a 440 μM solution of resazurin in PBS is added to each well of the plate and plates are incubated for an additional 5 h at 37℃, 5% CO2, and 95% humidity. Plates are read on a Synergy2 reader using an excitation of 540 nm and an emission of 600 nm. Data are analyzed using Prism software to calculate IC 50 values.(Only for Reference)
• Animal Research:
  Animal Models: Female NIH nude rats bearing BRAF V600E ST019VR PDX tumorsFormulation: 20% cyclodextrin, 25 mM phosphate, pH2.0Dosages: 30 mg/kgAdministration: p.o.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

DP 4978, DP4978, DP-4978, C-Raf, B-Raf (V600E), B-Raf (WT), Autophagy, LY 3009120, LY3009120, LY-3009120, inhibit, Inhibitor, Raf kinases, Raf

Compound Identifiers

PubChem CID

71721540